CO4950525A1 - Derivados de dolastatina 15 con funcionalidades carbonilo y heterociclicas en el c-terminal - Google Patents

Derivados de dolastatina 15 con funcionalidades carbonilo y heterociclicas en el c-terminal

Info

Publication number
CO4950525A1
CO4950525A1 CO98012757A CO98012757A CO4950525A1 CO 4950525 A1 CO4950525 A1 CO 4950525A1 CO 98012757 A CO98012757 A CO 98012757A CO 98012757 A CO98012757 A CO 98012757A CO 4950525 A1 CO4950525 A1 CO 4950525A1
Authority
CO
Colombia
Prior art keywords
acid
group
alkyl
compound
clause
Prior art date
Application number
CO98012757A
Other languages
English (en)
Inventor
Kurt Ritter
Wilhelm Amberg
Teresa Barlozzari
Andreas Haupt
Bernd Janssen
Andreas Kling
Original Assignee
Basf Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Basf Ag filed Critical Basf Ag
Publication of CO4950525A1 publication Critical patent/CO4950525A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
    • C07K5/101—Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1027—Tetrapeptides containing heteroatoms different from O, S, or N
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02—Linear peptides containing at least one abnormal peptide link
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Un compuesto, CARACTERIZADO PORQUE presenta la siguientefórmula general A-B-D-E-F-G, donde A, B, D y E son, cada uno, un residuo de un a-aminoácido; F es un residuo del ácido azacicloalcancarboxílico y G es un radical monovalente seleccionado del grupo formado por hidrógeno, alquilo, cicloalquilo, cicloalquilalquilo, amincarbonilalquilo, arilalquilo, alcoxicarbonilalquilo, ariloxicarbonilalquilo, alquilsulfinilalquilo, alquilsulfonilalquilo, arilsulfinilalquilo, arilsulfonilalquilo, alquil- o arilsulfinilo y alquil- o arilsulfonilo; o F es un grupo azacicloalquilo y G es un grupo heteroarilo; o una sal ácido de los mismos. El compuesto de la cláusula 1, CARACTERIZADO PORQUE el ácido es seleccionado del grupo formado por: ácido clorhídrico, ácido cítrico, ácido tartárico, ácido láctico, ácido fosfórico, ácido metansulfónico, ácido acético, ácido fórmico, ácido maléico, ácido fumárico, ácido málico, ácido succínico, ácido malónico, ácido sulfúrico, ácido L- glutámico, ácido L-aspártico, ácido pirúvico, ácido múcico, ácido benzóico, ácido glucurónico, ácido oxálico, ácido ascórbico o N-acetilglicina. El compuesto de la cláusula 1, CARACTERIZADO PORQUE A es un derivado de prolina de Fórmula IIa, na es 0, 1, 2 ó 9 3; Ra es un átomo de hidrógeno o un grupo metilo, etilo, propilo normal, isopropilo o ciclopropilo no sustituido o sustituido con flúor, R1 a es un átomo de hidrógeno o un grupo metilo, etilo, propilo, fenilo o grupo fenilo sustituido, donde los sustituyentes de fenilo comprenden uno o más grupos alquilo, alcoxi, trifluorometilo o ...
CO98012757A 1997-03-10 1998-03-09 Derivados de dolastatina 15 con funcionalidades carbonilo y heterociclicas en el c-terminal CO4950525A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US08/814,577 US5965537A (en) 1997-03-10 1997-03-10 Dolastatin 15 derivatives with carbonyl and heterocyclic functionalities at the C-terminus

Publications (1)

Publication Number Publication Date
CO4950525A1 true CO4950525A1 (es) 2000-09-01

Family

ID=25215470

Family Applications (1)

Application Number Title Priority Date Filing Date
CO98012757A CO4950525A1 (es) 1997-03-10 1998-03-09 Derivados de dolastatina 15 con funcionalidades carbonilo y heterociclicas en el c-terminal

Country Status (17)

Country Link
US (1) US5965537A (es)
EP (1) EP0981539A1 (es)
JP (1) JP2001518084A (es)
KR (1) KR20000076099A (es)
CN (1) CN1252806A (es)
AR (1) AR011957A1 (es)
AU (1) AU744511B2 (es)
BR (1) BR9808017A (es)
CA (1) CA2297164A1 (es)
CO (1) CO4950525A1 (es)
HR (1) HRP980124A2 (es)
HU (1) HUP0001758A3 (es)
IL (1) IL131596A0 (es)
NO (1) NO994364L (es)
TW (1) TW505657B (es)
WO (1) WO1998040400A1 (es)
ZA (1) ZA981957B (es)

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EP2266607A3 (en) 1999-10-01 2011-04-20 Immunogen, Inc. Immunoconjugates for treating cancer
US7125891B2 (en) * 2000-10-30 2006-10-24 Janssen Pharmaceutica N.V. Tripeptidyl peptidase inhibitors
US7256257B2 (en) * 2001-04-30 2007-08-14 Seattle Genetics, Inc. Pentapeptide compounds and uses related thereto
US6884869B2 (en) * 2001-04-30 2005-04-26 Seattle Genetics, Inc. Pentapeptide compounds and uses related thereto
EP2357006B1 (en) 2002-07-31 2015-09-16 Seattle Genetics, Inc. Drug conjugates and their use for treating cancer, an autoimmune disease or an infectious disease
DE10240818A1 (de) * 2002-08-30 2004-05-13 Grünenthal GmbH Substituierte 2-Pyrrolidin-2-yl-[1,3,4]-oxadiazol-Derivate
FR2856685B1 (fr) * 2003-06-25 2005-09-23 Merck Sante Sas Derives de thiazolylpiperidine, leurs procedes de preparation et les compositions pharmaceutiques qui les contiennent
BR122018071968B8 (pt) 2003-11-06 2021-07-27 Seattle Genetics Inc conjugado de anticorpo-droga, composição farmacêutica, artigo de manufatura e uso de um conjugado de anticorpo-droga
JP4954983B2 (ja) 2005-05-18 2012-06-20 ファーマサイエンス・インコーポレイテッド Ｂｉｒドメイン結合化合物
CN101535300B (zh) 2006-05-16 2014-05-28 埃格拉医疗公司 Iap bir域结合化合物
PE20140614A1 (es) 2007-07-16 2014-05-28 Genentech Inc Anticuerpos anti-cd79b e inmunoconjugados
AU2011215900A1 (en) 2010-02-10 2012-07-26 Immunogen, Inc. CD20 antibodies and uses thereof
WO2011098904A1 (en) 2010-02-12 2011-08-18 Aegera Therapeutics, Inc. Iap bir domain binding compounds
JP6133431B2 (ja) 2012-11-24 2017-05-24 ハンジョウ ディーエーシー バイオテック シーオー．，エルティディ．Ｈａｎｇｚｈｏｕ Ｄａｃ Ｂｉｏｔｅｃｈ Ｃｏ．，Ｌｔｄ． 親水性連結体及び薬物分子と細胞結合分子との共役反応における親水性連結体の使用
US10464955B2 (en) 2014-02-28 2019-11-05 Hangzhou Dac Biotech Co., Ltd. Charged linkers and their uses for conjugation
WO2016086357A1 (en) * 2014-12-02 2016-06-09 Merck Sharp & Dohme Corp. Methyl oxazole orexin receptor antagonists
US9987255B2 (en) 2014-12-19 2018-06-05 Merck Sharp & Dohme Corp. 5,5-bicyclic oxazole orexin receptor antagonists
CN104952808A (zh) * 2015-06-12 2015-09-30 广州先艺电子科技有限公司 一种预置金锡盖板及其制造方法
AU2015242213A1 (en) 2015-07-12 2018-03-08 Hangzhou Dac Biotech Co., Ltd Bridge linkers for conjugation of cell-binding molecules
US9839687B2 (en) 2015-07-15 2017-12-12 Suzhou M-Conj Biotech Co., Ltd. Acetylenedicarboxyl linkers and their uses in specific conjugation of a cell-binding molecule
KR20220147720A (ko) 2016-11-14 2022-11-03 항저우 디에이씨 바이오테크 씨오, 엘티디 결합 링커, 그러한 결합 링커를 함유하는 세포 결합 분자-약물 결합체, 링커를 갖는 그러한 결합체의 제조 및 사용
CN109776342A (zh) * 2019-02-26 2019-05-21 北京大学深圳研究生院 顺式β-氨基酸及其衍生物的合成方法
BR112022005289A2 (pt) * 2019-10-17 2022-09-20 Givaudan Sa Azaciclos substituídos como moduladores de trmp8
WO2023033129A1 (ja) 2021-09-03 2023-03-09 東レ株式会社 癌の治療及び／又は予防用医薬組成物

Family Cites Families (11)

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US4816444A (en) * 1987-07-10 1989-03-28 Arizona Board Of Regents, Arizona State University Cell growth inhibitory substance
US4879278A (en) * 1989-05-16 1989-11-07 Arizona Board Of Regents Isolation and structural elucidation of the cytostatic linear depsipeptide dolastatin 15
US5091368A (en) * 1990-08-08 1992-02-25 Harbor Branch Oceanographic Institution, Inc. Biologically active compounds from blue-green algae
DE69230824T2 (de) * 1991-08-09 2000-07-27 Teikoku Hormone Mfg Co Ltd Neue tetrapeptidderivate
UA45304C2 (uk) * 1992-05-20 2002-04-15 Басф Аг Похідні пептиду або їх солі, фармацевтична композиція
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US5504191A (en) * 1994-08-01 1996-04-02 Arizona Board Of Regents Acting On Behalf Of Arizona State University Human cancer inhibitory pentapeptide methyl esters
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US5554725A (en) * 1994-09-14 1996-09-10 Arizona Board Of Regents Acting On Behalf Of Arizona State University Synthesis of dolastatin 15
US5807984A (en) * 1995-11-09 1998-09-15 Basf Aktienegesellschaft Oligopeptides, the preparation and use thereof

Also Published As

Publication number Publication date
HUP0001758A2 (hu) 2001-05-28
AU6448298A (en) 1998-09-29
US5965537A (en) 1999-10-12
IL131596A0 (en) 2001-01-28
BR9808017A (pt) 2000-03-08
HUP0001758A3 (en) 2001-12-28
NO994364D0 (no) 1999-09-09
ZA981957B (en) 1999-09-09
CA2297164A1 (en) 1998-09-17
AU744511B2 (en) 2002-02-28
KR20000076099A (ko) 2000-12-26
HRP980124A2 (en) 1998-12-31
EP0981539A1 (en) 2000-03-01
JP2001518084A (ja) 2001-10-09
TW505657B (en) 2002-10-11
AR011957A1 (es) 2000-09-13
NO994364L (no) 1999-11-09
CN1252806A (zh) 2000-05-10
WO1998040400A1 (en) 1998-09-17

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